Solid Medicament Dosage Form Consumption Aid

ABSTRACT

A flavored, lubricating solution is applied to a solid medicament by spray, dipping, or otherwise coating the medicament. This liquid coating masks the often objectionable taste of the medicament while lubricating it, and thus significantly improving the ability to swallow the medicament. The improvement to the swallowing process is dramatically enhanced with significant reduction in gag reflex, general un-palatability and inability to move the dosage form completely through the mouth, palate, and esophagus to the stomach without sticking or lodging at any point in the process. The solution is a mixture of viscosity-adhesion-lubricity ingredients which includes polyols and polysaccharides, preservative agents, flavoring agents (to improve the palatability of the solution) and optional dispensing agents.

CROSS-REFERENCE TO PRIOR APPLICATIONS

Not Applicable

U.S. GOVERNMENT SUPPORT

Not Applicable

BACKGROUND OF THE INVENTION

1. Area of the Art

The present invention is in the area of oral medicaments and morespecifically an aid to facilitate the swallowing of solid medicaments.

2. Description of the Background Art

Overview of need: The inability to move a dosage of medicationcompletely through the mouth, palate and down esophagus to the stomachis a significant problem for most children, a large percentage ofgeriatric patients and a surprisingly high percentage of the generalpopulation. This is also a problem with ingestion of products forveterinary care. Obviously, if a patient is unable to swallow medicineor finds swallowing to be very uncomfortable, there is a significantlikelihood that patient will “forget” to take the medicine with oftenserious medical consequences.

There are both a physiological and a psychological aspects to theproblem. Although the process of swallowing is actually quite complexinvolving coordinated peristalsis of the muscles of the esophagus, theprocess is almost entirely automatic. However, various neurologicaldeficits can make proper swallowing difficult. In such cases the patientmay benefit from something that eases the swallowing process. Difficultyin swallowing may result in an uncomfortable feeling that something isstuck in the throat or chest. This may also involve an inability ordifficulty in breathing and a resulting choking or gagging reflex.Certainly, there is almost nothing more frightening than an inability tobreathe. As a result people who have had any difficulties in swallowingmay develop such fear or anxiety that the natural swallowing process iscompromised. Thus, a fear of swallowing difficulties may provoke actualswallowing difficulties. A treatment that eases swallowing will benefitsuch individuals in at least two ways. First, they will actually be ableto swallow needed medicaments. Second, after repeated instances ofsuccessful swallowing, their anxiety about swallowing will abate andthey will continue to enjoy improved swallowing ability.

Physicians often provide a number of tips concerning swallowingincluding chewing one's food thoroughly and ingesting foods that arelargely liquid. This advice, however, does little to help withswallowing solid medicaments. One can hardly chew a pill thoroughly, andalthough a pill can be powdered, this may alter the proper uptake of thedrug and will often result in a truly foul tasting mixture—somethingthat causes a patient to be even less likely to take medications asprescribed. In many cases drugs can be compounded in a liquid form, butwith a significant number of pharmaceuticals a liquid dosage is eithernot possible or at least not practical. Although pharmacists can make upa liquid form of many solid drugs, in a number of cases the liquiddosages are significantly less stable than the solid drug. Often thepatient is required to refrigerate the liquid drug solution, and eventhen full stability and activity is not assured.

This problem is known in the art and a number of attempts have been madeto solve it. One popular approach has been to develop coatings for pillsand other solid medicaments that facilitate swallowing. For example,U.S. Pat. No. 4,863,741 to Becker describes an enteric coating thatfacilitates swallowing. U.S. Patent Application No. 2005/0025825 toHeasley et al. describes another coating intended to improve swallowing.Another approach used in the art has been to modify the tried and truemethod of taking a drink of water to help with swallowing. There are anumber of disclosures which modify the viscosity of the liquid used toaid in swallowing. See for example, U.S. Pat. No. 6,277,395 to Fukui etal. which discloses a somewhat viscous drink that apparently helps holdthe esophagus open during the swallowing process. However, it does notappear that the art has used a thin liquid coating containingviscosity-adhesion-lubricity agents as opposed to a modified liquid thatfills the esophagus around the medicament.

SUMMARY OF THE INVENTION

A flavored, lubricating solution is applied to the solid dosage byspray, dipping, or otherwise coating the medicament. This liquid coatingmasks the often objectionable taste of the medicament while lubricatingthe dosage and thus significantly improving the ability to swallow themedicament. The improvement to the swallowing process is dramaticallyenhanced with significant reduction in gag reflex, generalun-palatability and inability to move the dosage form completely throughthe mouth, palate, and esophagus to the stomach without sticking orlodging at any point in the process. This liquid lubricant can also aidin placement of tubes through the oral and nasal cavities commonlyreferred to as NG tubes, gastric tubes and other similar devices used inmedical practice.

The solution is a mixture of viscosity-adhesion-lubricity ingredientswhich includes polyols and polysaccharides, preservative agents,flavoring agents (to improve the palatability of the solution) andoptional dispensing agents. The viscosity-adhesion-lubricity agents playa central role by adhering to and coating the solid medicament. At thesame time these materials are slippery so that the coated medicament canslide down the patient's throat without causing discomfort or gagging.The pleasant sensation of using the solution is further enhanced by theflavoring agents which are generally sweet and mask any unpleasant tastefrom the medicament. The dispensing agents may be added to reducefoaming or other characteristics which might interfere with applicationof the solution. The preservative agents are included to prevent anyinadvertent microbiological contamination of the solution.

DETAILED DESCRIPTION OF THE INVENTION

The following description is provided to enable any person skilled inthe art to make and use the invention and sets forth the best modescontemplated by the inventor of carrying out his invention. Variousmodifications, however, will remain readily apparent to those skilled inthe art, since the general principles of the present invention have beendefined herein specifically to provide a liquid to be applied to a solidmedicament to improve swallowing of the medicament

Ingredients: The inventive swallowing aid is a water-based liquid madewith purified water. Generally speaking the mixture containsviscosity-adhesion-lubricity (VAL) modifying agents, flavoring agents,dispensing agents and preservative agents. The VAL agents cause theliquid mixture to coat and adhere to the solid medicament. The VALagents may also provide a lubricating properties. The flavoring agentsare provided to mask unpleasant tastes of medicaments and includesweetening agents. The dispensing agents further modify the physicalcharacteristics of the mixture and make it easier to dispense (e.g.,preventing foam formation) and may also contribute to medicament coatingas in the case of an added surfactant. The preservative agents preventmicrobial growth should the mixture become contaminated.

The VAL ingredients are quite important to the end product. One aspectof the product is adding slipperiness or lubricity to the medicament soit readily passes down the throat. For the lubricity to be effective,the product must evenly coat and adhere to the medicament. Often thesurface of a pill is so smooth that an otherwise effective mixture beadup and leave areas of the pill uncoated. This may contribute to stickingof the pill with resulting gagging and general unpleasantness.Surfactants and VAL ingredients improve adhesion-adherence and evencoating properties of the product. Increasing the viscosity may alsohelp because a thicker liquid is less likely to bead up. However, theproduct must not be so viscous as to be sticky and thereby actuallyimpede swallowing.

It should be appreciated that some ingredients may serve more than onefunction. For example, a sugar alcohol such a sorbitol can be used tomodify viscosity and provide lubricity, but since this material is alsosomewhat sweet in taste, it also acts as a flavoring agent. VAL agentsinclude mostly hydrophilic molecules such as sorbitol (including othersugar alcohols such as galactitol, erythritol, inositol, maltitol,mannitol, ribitol, and xylitol) glycerin, other polyols such aspropylene glycol and polyethylene glycol, and polysaccharides such asxanthan gum, carboxymethylcellulose, alginate and carregenan. Otherplant gums and cellulose ethers may also be used. Microcrystallinecellulose is a somewhat usual material that can enhance the VAL agents.Microcrystalline cellulose is not soluble per se and contributes opacityto the formula (if so desired). It also contributes viscosity andadhesion of the formula.

Materials like citric acid and sodium citrate generally contribute tothe product characteristics and can be considered a flavoring agent(adding tartness). Simethacone, an antifoaming agent, is a usefuldispensing agent. Preservative agents include citric acid/sodiumcitrate, sulfites, propionic acid, methylparaben, propylparaben,benzoates and sorbates, EDTA (ethylene-diamine-tetraacetic acid) andother food grade preservatives known to those of ordinary skill in theart of food science. Many additional preservatives are known to those ofordinary skill in food sciences. Flavoring agents include the usualessential oils and usual fruit flavors. Flavoring agents also includeartificial sweeteners such as aspartame, acesulfame, sucralose, andneotame. A preferred formulation is made with FDA approved ingredientsand is alcohol free and sugar free.

The actual final formulation will depend on how the product is to bedispensed (i.e., applied to the medicament). Application methods includepouring, dipping, brushing and spraying. I have found that sprayingappears to be the most successful application method. Dipping andbrushing have the drawback of transferring bits of the medicament intothe product container. In addition, microorganisms are readilytransferred into the container. Although the preservative agents areincluded to prevent growth of microorganisms, it is sensible to avoidcontamination as much as possible. Pouring wastes product and oftenfails to evenly coat the medicament. Therefore, a preferred method ofapplication is to place the product in a small pump sprayer such asthose sold for applying cleaning fluid to glasses. Formulations intendedfor spray application need to have a low enough viscosity to permitready spraying. Methods of application such as pouring can useconsiderably more viscous formulations.

I have found that a good formula for spray application consists of anaqueous solution of a sugar alcohol and low molecular weight polyol suchas glycerin together with a small quantity of preservative and flavoringagent. Both the glycerol and sugar alcohol act as VAL agents and alsoact as sweeteners. A 50% solution of glycerin has a viscosity around 6centipoises. A 45% solution of sorbitol has a viscosity of about 170centipoises so it can be seen that sugar alcohols generally contributemore to the viscosity. A workable formula consists of about 30% to 80%by weight VAL with the remaining weight being water. A usable VALcomposition comprises sorbitol between about 0% and 40% and glycerinbetween about 25% and about 75%. Decreasing the amount of sorbitolreduces the viscosity and somewhat decreases adhesion and coating whileat the same time decreasing the overall sweetness of the product (lackof sweetness, however, can be corrected with artificial sweeteners).However, because sorbitol is more expensive than glycerin, manufacturingcost also decrease. The final mixture also contains a small amount(usually less than 1% by weight) of flavoring agent and preservativeagent.

A preferred method of using this formulation is to spray the pill orother medicament prior to insertion in the mouth. The pill can besprayed in a small cup (or similar container) and then picked up andplaced into the mouth. Alternatively, the pill can be placed on the palmof the hand and sprayed; however, some users object to having theslippery product on their hands. In most cases liquid like water is usedto help swallow the coated medicament. The hydrophilic formula hassufficient viscosity and adhering properties to not be washed off themedicament when the medicament is swallowed with water. In some casesthe product works so well that patients have little difficulty inswallowing the medicament without a glass of water.

Product testing results: The product was given to more than thirtyhealthy and swallowing compromised test subjects from the ages of 4 to90 years. All were instructed on application by spray and consumption.All test subjects reported significant improvement to the palatabilityof the medicaments they were consuming and most importantly reporteddramatic improvement to the successful ingestion without complicationdue to the improved lubricity and pre-wetting of the medicament with theadhering solution. The most dramatic improvement was obvious not withthe segment of the test subjects who essentially had no significantdifficulty with ingestion but rather those individuals that normallydisplayed an inability to ingest solid medicaments. These subjectsrepresented about 10% of the test population. The most gratifyingoutcome of the test was that these individuals experienced such dramaticimprovements to the quality of life in this respect that they haveinsisted on continued use of the product after the tests were completed.Several subjects reported the ability to swallow tablets and capsules inlarge numbers even without water. It is anticipated that the formulawill work well for veterinary medicaments (albeit with, perhaps, adifferent flavoring agent), and veterinary tests are ongoing.

The following claims are thus to be understood to include what isspecifically illustrated and described above, what is conceptuallyequivalent, what can be obviously substituted and also what essentiallyincorporates the essential idea of the invention. Those skilled in theart will appreciate that various adaptations and modifications of thejust-described preferred embodiment can be configured without departingfrom the scope of the invention. The illustrated embodiment has been setforth only for the purposes of example and that should not be taken aslimiting the invention. Therefore, it is to be understood that, withinthe scope of the appended claims, the invention may be practiced otherthan as specifically described herein.

1. A liquid formula for application to a solid medicament comprising: aviscosity-adhesion-lubricity agent selected from the group consisting ofsugar alcohols, polyols, polysaccharides and mixtures thereof, flavoringagents; and purified water.
 2. The liquid formula according to claim 1further comprising a preservative agent.
 3. The liquid formula accordingto claim 2, wherein the preservative agent is selected from the groupconsisting of citric acid, sodium citrate, sulfites, propionic acid,methylparaben, propylparaben, benzoates, sorbates, and EDTA.
 4. Theliquid formula according to claim 1, wherein the flavoring agentcomprises a sugar alcohol.
 5. The liquid formula according to claim 1,wherein the sugar alcohol is selected from the group consisting ofgalactitol, erythritol, inositol, maltitol, mannitol, ribitol, sorbitoland xylitol.
 6. The liquid formula according to claim 1, wherein thepolyol is selected from the group consisting of glycerin, propyleneglycol and polyethylene glycol.
 7. The liquid formula according to claim1, wherein the polysaccharide is selected from the group consisting ofxanthan gum, carboxymethylcellulose, alginate and carregenan.
 8. Theliquid formula according to claim 6, wherein the polysaccharide furthercomprises microcrystalline cellulose.
 9. A liquid formula forapplication to a solid medicament comprising: aviscosity-adhesion-lubricity agent which comprises between about 0% andabout 40% by weight sorbitol and about 25% and about 75% by weightglycerin; flavoring agents; and purified water.
 10. The liquid formulaaccording to claim 9, wherein the flavoring agents comprise sorbitol.11. The liquid formula according to claim 9 further comprising anartificial sweetener.
 12. The liquid formula according to claim 9further comprising a preservative agent.
 13. A method for facilitatingthe swallowing of a solid medicament comprising the steps of: providinga sprayer containing an aqueous solution of aviscosity-adhesion-lubricity agent; operating the sprayer to coat asolid medicament with the aqueous solution; and ingesting the coatedmedicament whereby swallowing the medicament is facilitated.
 14. Themethod according to claim 13, wherein the aqueous solution furthercomprises an artificial sweetener.
 15. The method according to claim 13,wherein the aqueous solution further comprises a preservative agent. 16.The method according to claim 2, wherein the preservative agent isselected from the group consisting of citric acid, sodium citrate,sulfites, propionic acid, methylparaben, propylparaben, benzoates,sorbates, and EDTA.
 17. The method according to claim 13, wherein theaqueous solution further comprises a flavoring agent.
 18. The methodaccording to claim 13, wherein the viscosity-adhesion-lubricity agentcomprises a sugar alcohol selected from the group consisting ofgalactitol, erythritol, inositol, maltitol, mannitol, ribitol, sorbitoland xylitol.
 19. The method according to claim 13, wherein theviscosity-adhesion-lubricity agent comprises a polyol selected from thegroup consisting of glycerin, propylene glycol and polyethylene glycol.20. The method according to claim 13, wherein theviscosity-adhesion-lubricity agent comprises a polysaccharide selectedfrom the group consisting of xanthan gum, carboxymethylcellulose,alginate and carregenan.